Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.
Article Details
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Knuckley B, Luo Y, Thompson PR
Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors.
Bioorg Med Chem. 2008 Jan 15;16(2):739-45. Epub 2007 Oct 13.
- PubMed ID
- 17964793 [ View in PubMed]
- Abstract
Protein Arginine Deiminase 4 (PAD4) has emerged as a leading target for the development of a Rheumatoid Arthritis (RA) pharmaceutical. Herein, we describe the development of a novel screen for PAD4 inhibitors that is based on a PAD4-targeted Activity-Based Protein Profiling reagent, denoted Rhodamine-conjugated F-Amidine (RFA). This screen was validated by screening 10 Disease Modifying Anti-Rheumatic Drugs (DMARDs) and identified streptomycin, minocycline, and chlortetracycline as micromolar inhibitors of PAD4 activity.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Azithromycin Protein-arginine deiminase type-4 Protein Humans UnknownInhibitorDetails Chlortetracycline Protein-arginine deiminase type-4 Protein Humans UnknownInhibitorDetails Streptomycin Protein-arginine deiminase type-4 Protein Humans NoInhibitorDetails Tetracycline Protein-arginine deiminase type-4 Protein Humans UnknownNot Available Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Azithromycin Protein-arginine deiminase type-4 IC 50 (nM) >10000000 N/A N/A Details Tetracycline Protein-arginine deiminase type-4 IC 50 (nM) 780000 N/A N/A Details